| 15th week of 2015 patent applcation highlights part 37 |
| Patent application number | Title | Published |
|---|
| 20150099698 | COMBINATION PEPTIDE-NANOPARTICLES AND DELIVERY SYSTEMS INCORPORATING SAME - Nanoparticles having a core and a corona of ligands covalently linked to the core, wherein differing species of peptides are bound to the nanoparticles and incorporated into various dosage forms. | 2015-04-09 |
| 20150099699 | CONJUGATES OF INSULIN-LIKE GROWTH FACTOR-1 AND POLY(ETHYLENE GLYCOL) - A conjugate consisting of an insulin-like growth factor-1 (IGF-I) variant and one or two poly(ethylene glycol) group(s), characterized in that said IGF-I variant has an amino acid alteration at up to three amino acid positions 27, 37, 65, 68 of the wild-type IGF-I amino acid sequence so that one or two of said amino acids is/are lysine and amino acid 27 is a polar amino acid but not lysine, is conjugated via the primary amino group(s) of said lysine(s) and said poly(ethylene glycol) group(s) have an overall molecular weight of from 20 to 100 kDa is disclosed. This conjugate is useful for the treatment of neurodegenerative disorders like Alzheimer's Disease. | 2015-04-09 |
| 20150099700 | METHODS FOR DETECTING PROGENITOR CELLS AND USES THEREOF - Diagnostic and therapeutic methods pertaining to diseases and disorders of the breast, uterus and ovary are encompassed herein. More particularly, diagnostic methods for early detection of progenitor cells of breast, uterine, and ovarian cancers are described herein. The identification of markers for these cancer predisposing progenitor cells, which co-express the progesterone receptor (PR) and p63, provides tools and methods of use thereof that facilitate early detection of increased frequency of PR/p63 double positive (PR/p63+) progenitor cells in asymptomatic patients and thus, early detection of increased cancer risk in such patients and assessment, diagnostic stratification, and evaluation of therapeutic intervention in symptomatic patients. Therapeutic methods are also encompassed herein, which include detection of PR/p63+ progenitor cells in a patient, wherein detection of increased frequency of PR/p63+ progenitor cells provides information on which basis a determination of therapeutic regimen or an assessment of an ongoing therapeutic regimen can be made. | 2015-04-09 |
| 20150099701 | MODIFIED ACIDIC FIBROBLAST GROWTH FACTORS AND COMPOSITION THEREOF - The present invention provides acidic fibroblast growth factor (aFGF) composition, comprising: (i) aFGF of SEQ ID NO: 1, (ii) aFGF of SEQ ID NO: 1 having an N-terminal phosphogluconoylation, (iii) aFGF of SEQ ID NO: 1 having an N-terminal gluconoylation, (iv) aFGF of SEQ ID NO: 2 and (v) aFGF of SEQ ID NO: 3, or a combination thereof. Also provided is a modified acidic fibroblast growth factor (aFGF) which has an N-terminal phosphogluconoylation or gluconoylation. | 2015-04-09 |
| 20150099702 | USE OF RNA INTERFEARENCE, FARNESOIC ACID AND RECOMBINANT PROTEIN APPROACH TO INDUCE GONAD MATURATION IN CRUSTACEAN SPECIES - This invention is directed to the compositions and methods for inducing female gonad maturation in crustacean species such as shrimp, lobster or crab. In one embodiment, the composition for inducing gonad maturation comprises a dsRNA corresponding to the GIH DNA, recombinant protein of a gonad stimulatory hormone (GSH) and farnesoic acid (FA). In another embodiment, the composition for inducing gonad maturation comprises a dsRNA corresponding to the GIH DNA, recombinant MeMIH-B protein and farnesoic acid (FA). | 2015-04-09 |
| 20150099703 | TREATMENT OF POSTPARTUM HAEMORRHAGE WITH CHEMICALLY MODIFIED HEPARIN OR HEPARAN SULPHATE AND A UTEROTONIC AGENT - The present invention refers to the use of certain sulfated glycosaminoglycans for treatment or prevention of postpartum haemorrhage. The sulfated glycosaminoglycans have a reduced anticoagulant activity and are administered in combination with at least one uterotonic agent capable of promoting myometrial contractions of the uterus and thereby compress the vessels and cease the bleeding. | 2015-04-09 |
| 20150099704 | Peptide Inhibitors of Calcium Oxalate Monohydrate Crystallization and Uses Thereof - In an embodiment, the present disclosure pertains to a composition for inhibiting calcium oxalate monohydrate crystal growth comprising at least one isolated polypeptide comprising a plurality of amino acids that bind the surface of the calcium oxalate monohydrate crystal; and a plurality of amino acids spacers, wherein the amino acid spacers are arranged in varying sequences between the plurality of amino acids that bind the surface of the calcium oxalate monohydrate crystal. In some embodiments, the present disclosure related to a method of controlling calcium oxalate monohydrate crystal growth in a subject in need thereof comprising administering to the subject therapeutically effective amount of the calcium oxalate monohydrate inhibiting polypeptide. In some embodiments, the present disclosure relates to a method of identifying calcium oxalate monohydrate inhibiting peptides. Such a method may comprise designing a peptide library of potential calcium oxalate inhibiting peptides; screening the peptide library for high efficacy inhibitor peptides for inhibition of calcium oxalate monohydrate crystallization; and conducting molecular characterization of the high efficacy inhibitor to determine specificity. | 2015-04-09 |
| 20150099705 | PROTOXIN -II VARIANTS AND METHODS OF USE - The present invention relates to Protoxin-II variants, polynucleotides encoding them, and methods of making and using the foregoing. | 2015-04-09 |
| 20150099706 | TREATMENT OF ISCHEMIC STROKE WITH DRa1-MOG-35-55 - Methods and compositions used in treating ischemic stroke using a recombinant DRα-MOG-35-55 construct are disclosed. The disclosed methods involve administering a pharmaceutical composition comprising DRα-MOG-35-55 and a pharmaceutically acceptable carrier to a subject that has had or is at risk of developing ischemic stroke. | 2015-04-09 |
| 20150099707 | MODIFIED PSEUDOMONAS EXOTOXIN A - The invention provides a | 2015-04-09 |
| 20150099708 | WNT COMPOSITIONS AND THERAPEUTIC USES OF SUCH COMPOSITIONS - The invention provides novel Wnt polypeptides that have improved production characteristics, solubility, systemic delivery, and tissue uptake, and polynucleotides encoding the Wnt polypeptides of the invention. The Wnt polypeptides of the invention can be used therapeutically, such as, for example, in methods of preventing or treating muscle loss and/or promoting muscle hypertrophy and growth. | 2015-04-09 |
| 20150099709 | GHRELIN RECEPTOR AGONISTS FOR THE TREATMENT OF ACHLORHYDRIA - The present invention relates to a use of a compound having ghrelin receptor agonistic activity, a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof for the manufacture of a medicament for treatment of diseases including achlorhydria in which abnormal gastric acid secretion is involved. In addition, the present invention relates to the method of treatment including administering to a human or animal. The compound, the pharmaceutically acceptable salt thereof, or pharmaceutical compositions containing them, may be used in combination with one or more second active agents. Further, the present invention relates to pharmaceutical compositions and kits comprising a compound of the present invention or a pharmaceutically acceptable salt thereof for the treatment of said diseases. | 2015-04-09 |
| 20150099710 | Feed Additive, Feed, and Method for Producing Feed - Objects are to provide an additive for a feed which can improve growth performance and meat quality of livestock, and can improve palatability of the feed, a feed and a method for preparing the feed, and the objects can be solved by an additive for a feed which comprises at least one or two or more of a polyphenol derived from EFB, α-tocopherol derived from EFB and xyloses derived from EFB, a feed which comprises an additive for a feed being added to a formulating material for a feed in the range of 0.05 to 20% by weight with a dry basis, and a method for preparing the feed. | 2015-04-09 |
| 20150099711 | METHOD AND SYSTEM FOR MODIFYING RAW FOODS, AND RAW FOOD PRODUCT MADE THEREBY - A method for modifying a quality of a fruit includes cutting a live stem attached to a live fruit at a cut distance from the fruit, producing a cut end of the stem, contacting only the cut end of the stem with a solution comprising at least one mobile and quality-modifying food ingredient while protecting the fruit from contact with the solution, and keeping the cut end of the stem in contact with the solution for an incubation time sufficient to allow absorption and transport of the food ingredient into the fruit, the food ingredient conferring a modified quality upon the fruit. A system for practicing the method and an edible raw plant product produced by the method are also disclosed. | 2015-04-09 |
| 20150099712 | METHOD AND COMPOUNDS FOR INHIBITING THE MCM COMPLEX AND THEIR APPLICATION IN CANCER TREATMENT - A method for treating cancer by using an agent which is capable of inhibiting the functionality of the MCM complex, a heterohexameric ring formed from six subunits, in the process of DNA replication and a method of screening for such agents by detecting the locations and functions of the MCM subunits, such as hMcm2 and hMcm6, in cells treated with candidate compounds. | 2015-04-09 |
| 20150099713 | METHOD OF TREATING CONSTIPATION-PREDOMINANT IRRITABLE BOWEL SYNDROME - Disclosed is a method of manipulating the rate of gastrointestinal transit in a mammalian subject. Also disclosed is the use, in the manufactiurc of a medicament for the treatment of constipation, of a selective inhibitor of methanogensis, a methanogen-displacing probiotic agent, or a prebiotic agent that inhibits the growth of methanogenic bacteria or promotes the growth of competing non-methanogenic intestinal flora. Alternatively, in accordance with the invention, is disclosed the use in the manufacture of a medicament for the treatment of diarrhea, of methane or a methane precursor, a methanogenic or other methane-enhancing probiotic agent, or a methanogenesis-enhancing prebiotic agent. | 2015-04-09 |
| 20150099714 | SYNTHESIS OF DEUTERATED MORPHOLINE DERIVATIVES - The present invention is directed to a process for preparing a 2,26,6-d | 2015-04-09 |
| 20150099715 | FORMULATIONS OF ACADESINE - This invention provides a buffered solution comprising acadesine, as well as compositions, formulations and kits containing said solution. The solution, compositions, formulation, and kits can be used to prevent morbidity/mortality in a patient or to treat an ischaemic condition, a condition regulated by adenosine, or a condition associated with reduced blood flow to a tissue in a patient. | 2015-04-09 |
| 20150099716 | Maintenance of Platelet Inhibition During Antiplatelet Therapy - A method for reducing or maintaining platelet inhibition in a patient by administering cangrelor prior to an invasive procedure is described. The method of this invention can be used for patients in need of antiplatelet therapy or at risk of thrombosis. The method can further be used in patients who were previously treated with long-acting platelet inhibitors without increasing the risk of excessive bleeding. | 2015-04-09 |
| 20150099717 | METHODS AND KITS FOR TREATING VAGINAL AND VULVAR VESTIBULE MUCOSA DISORDERS - A method of treating a vaginal or vulvar vestibule mucosa disorder involves administering a composition comprising a hyaluronic acid or a salt thereof to the vagina, vulvar or vulvar vestibule of an individual that has the disorder to treat the disorder. The method may be used to treat vaginal atrophy or vulvar vestibulitis syndrome, among other vulvovaginal mucosa disorders. | 2015-04-09 |
| 20150099718 | HEPARIN-BASED COMPOSITIONS AND METHODS FOR THE INHIBITION OF METASTASIS - The invention provides the use in combination of a heparin containing composition that has anticoagulant activity when used alone, such as an unfractionated heparin or low molecular weight heparin, in combination with an inhibitor of the anticoagulation activity/effect or effect of heparin, for the inhibition of metastasis. | 2015-04-09 |
| 20150099719 | CATHEPSIN CYSTEINE PROTEASE INHIBITORS - This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis. | 2015-04-09 |
| 20150099720 | ANDROGEN RECEPTOR MODULATOR COMPOUNDS AND METHODS - Provided herein are compounds having a structure selected from among Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V) and Formula (VI) that are androgen receptor modulators and/or androgen receptor binding agents. Also disclosed are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions. | 2015-04-09 |
| 20150099721 | TREATING CANCER WITH HSP90 INHIBITORY COMPOUNDS - A method for treating cancer with a mutation in ROS or RET, comprising identifying a subject with a cancer with a mutation in ROS or RET, and administering to the subject an effective amount of a compound according to formulae (I) OR (la) or a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables structural formulae are defined herein. | 2015-04-09 |
| 20150099722 | 6-OXOPURINE PHOSPHORIBOSYLTRANSFERASE INHIBITORS - The invention relates to compounds which are useful as inhibitors of 6-oxopurine phosphoribosyltransferases such as hypoxanthine-guanine-(xanthine) phosphoribosyltransferase (HG(X)PRT). | 2015-04-09 |
| 20150099723 | FATTY ACID ACETYLATED SALICYLATES AND THEIR USES - The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative. | 2015-04-09 |
| 20150099724 | Novel crystals and process of making 5-(-methyl)-2-methoxy-benzoic acid - The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid. | 2015-04-09 |
| 20150099725 | TREATMENT OF ALLERGIC RHINITIS USING A COMBINATION OF MOMETASONE AND OLOPATADINE - The present patent application relates to a method of treating allergic rhinitis in a subject (preferably a human) by administering a combination of mometasone or its salt and olopatadine or its salt. | 2015-04-09 |
| 20150099726 | DRY POWDER INHALER - This invention provides a dry powder inhaler comprising: a dry powder medicament comprising fluticasone propionate, salmeterol xinafoate and a lactose carrier; wherein, the delivered dose of salmeterol per actuation is less than 50 μg; and wherein the dose provides a baseline-adjusted FEV | 2015-04-09 |
| 20150099727 | Aminosteroids for the Treatment of a PTP1B Associated Disease - This application is directed to the use of aminosteroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes. | 2015-04-09 |
| 20150099728 | Substituted Phenylureas and Phenylamides as Vanilloid Receptor Ligands - Substituted phenylureas and phenylamides, processes for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for preparing pharmaceutical compositions. | 2015-04-09 |
| 20150099729 | INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL - The present invention provides compounds of Formula I | 2015-04-09 |
| 20150099730 | IMIDAZOLIN-5-ONE DERIVATIVE USEFUL AS FASN INHIBITORS FOR THE TREATMENT OF CANCER - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: | 2015-04-09 |
| 20150099731 | USE OF PARTHENOLIDE DERIVATIVES AS ANTILEUKEMIC AND CYTOTOXIC AGENTS - The present invention provides compounds of the formula (I) | 2015-04-09 |
| 20150099732 | 3-ARYL-5-SUBSTITUTED-ISOQUINOLIN-1-ONE COMPOUNDS AND THEIR THERAPEUTIC USE - The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2H-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc. | 2015-04-09 |
| 20150099733 | HETEROARYLCARBOXYLIC ACID ESTER DERIVATIVE - Compounds represented by the following formula (I); | 2015-04-09 |
| 20150099734 | NEW DIAZASPIROCYCLOALKANE AND AZASPIROCYCLOALKANE - The invention provides novel compounds having the general formula (I) | 2015-04-09 |
| 20150099735 | TRIAZOLOPYRIDINE COMPOUNDS - The invention is concerned with triazolopyridine compounds of formula (I) | 2015-04-09 |
| 20150099736 | Indolyl-Pyridone Derivatives Having Checkpoint Kinase 1 Inhibitory Activity - Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: | 2015-04-09 |
| 20150099737 | PYRROLOPYRIMIDINE COMPOUNDS AS INHIBITORS OF CDK4/6 - The invention is directed to novel pyrrolopyrimidine compounds of formula (1) wherein R | 2015-04-09 |
| 20150099738 | ISOXAZOLINES AS INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provides isoxazoline FAAH inhibitors of the formula (I): | 2015-04-09 |
| 20150099739 | MODIFIED RELEASE PREPARATIONS CONTAINING OXCARBAZEPINE AND DERIVATIVES THEREOF - Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility- and/or release enhancing agents to provide tailored drug release profiles, preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed. | 2015-04-09 |
| 20150099740 | TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS - A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-β-hydroxysteroid dehydrogenase Type 1 enzyme activity. | 2015-04-09 |
| 20150099741 | DIAGNOSING AND TREATING PATIENTS HAVING PSYCHIATRIC DISORDERS - Disclosed are methods and kits for diagnosing, prognosing, and treating patients having psychiatric disorders. The methods may include assessing whether a patient has a treatment resistant psychiatric disorder or assessing whether the patient is likely to develop a treatment resistant psychiatric disorder. The methods may include detecting genetic markers such as the single nucleotide polymorphism (SNP) in genes present in a genomic nucleic acid sample from the patient, and/or receiving, as a caregiver, the results of tests indicating whether the genetic markers are present in the genomic nucleic acid sample from the patient. The methods may include administering treatment to the patient, for example, based on the detected genetic markers, and administering treatment may include administering new antipsychotic drugs (APDs) that are trace amine-associated receptor 1 (TAAR1) agonists. | 2015-04-09 |
| 20150099742 | PHANTOM PHENOMENA TREATMENT - The present invention relates to a substance for the treatment of the phantom phenomena of tinnitus and/or phantom pain, a method for the diagnosis and for the treatment of these phantom phenomena. | 2015-04-09 |
| 20150099743 | NOVEL N-PYRIMIDIN-4-YL-3-AMINO-PYRROLO[3,4-C]PYRAZOLE DERIVATIVES AS PKC KINASE INHIBITORS - The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: | 2015-04-09 |
| 20150099744 | COMBINATIONS OF HISTONE DEACETYLASE INHIBITORS AND EITHER HER2 INHIBITORS OR PI3K INHIBITORS - The invention relates to combinations comprising an HDAC inhibitor and a Her2 inhibitor for the treatrent of breast cancer in a subject in need thereof. The invention also relates to combinations comprising an HDAC inhibitor and a PI3K inhibitor for the treatment of breast cancer in a subject in need thereof. Also provided herein are methods for treating breast cancer in a subject in need thereof comprising administering to the subject an effective amount of one of the above combinations. Further provided are methods for inhibiting migration and/or invasion of a breast cancer cell in a subject by administering to the subject a HDAC6 specific inhibitor. | 2015-04-09 |
| 20150099745 | FORMULATIONS OF (S)-3-(4-((4-(MORPHOLINOMETHYL)BENZYL)OXY)-1-OXOISOINDOLIN-2-YL)PIPERIDIN- E-2,6-DIONE - Pharmaceutical compositions and single unit dosage forms of (S)-3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a pharmaceutically acceptable stereoisomer, prodrug, salt, solvate, hydrate, or clathrate, are provided herein. Also provided are methods of treating, managing, or preventing various disorders, such as cancer, an inflammatory disease and/or an immune-related disorder. | 2015-04-09 |
| 20150099746 | SUBSTITUTED 3-(5-MEMBERED UNSATURATED HETEROCYCLYL-1, 3-DIHYDRO-INDOL-2-ONE'S AND DERIVATIVES THEREOF AS KINASE INHIBITORS - The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. | 2015-04-09 |
| 20150099747 | Methods and Compositions For Detecting Mutation in the Human EZH2 Gene - The invention comprises reagents and methods for detecting cancer-associated mutations in the human EZH2 gene. Further, a method of detecting the mutations and a method of treatment are disclosed. | 2015-04-09 |
| 20150099748 | MULTIHETEROARYL COMPOUNDS AS INHIBITORS OF H-PGDS AND THEIR USE FOR TREATING PROSTAGLANDIN D2 MEDIATED DISEASES - Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D | 2015-04-09 |
| 20150099749 | HIV INHIBITING 5-AMIDO SUBSTITUTED PYRIMIDINES - This invention concerns pyrimidine derivatives of formula | 2015-04-09 |
| 20150099750 | METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. | 2015-04-09 |
| 20150099751 | IN SITU GEL LOADED WITH PHOSPHODIESTERASE TYPE V INHIBITORS NANOEMULSION - The in situ gel loaded with phosphodiesterase Type V (PDE5) inhibitors nanoemulsion was prepared using an innovative approach to reformulate the PDE5 inhibitors in a nanoemulsion, and then loading the nanoemulsion into an in situ gel base. These preparations are administered by intramuscular injection in order to give a depot effect for a period of time that exceeds 15 days. The in situ gel composition gives slow, controlled release of the PDE5 inhibitor. The in situ gel composition is useful for prophylaxis and treatment of some important chronic diseases, such as diabetic complications, benign prostatic hyperplasia, erectile dysfunction, and diseases associated with endothelial dysfunction. | 2015-04-09 |
| 20150099752 | PYRROLOTRIAZINONE DERIVATIVES AS PI3K INHIBITORS - New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks). | 2015-04-09 |
| 20150099753 | FORM 5 POLYMORPH OF 7-(TERT-BUTYL-D9)-3-(2,5-DIFLUOROPHENYL)-6-((1-METHYL-1H-1,2,4-TRIAZOL-5-- YL)METHOXY)-[1,2,4]TRIAZOLO[4,3-B]PYRIDAZINE - The present invention provides individual crystalline polymorphs of 7-(tert-Butyl-d9)-3-(2,5-difluorophenyl)-6-((1-methyl-1H-1,2,4-triazol-5-yl)methoxy)-[1,2,4]triazolo[4,3-b]pyridazine designated Form 5. The Form 5 polymorph disclosed herein is characterized according to one or more of (a) powder X-ray diffraction data (“XRPD”); (b) differential scanning calorimetry (“DSC”); (c) FT-Raman spectroscopy; (d) FT-IR spectroscopy; and (e) thermogravimetric analysis (TGA). | 2015-04-09 |
| 20150099754 | TREATMENT OF CANCER CHARACTERIZED BY GENE MUTATIONS - Provided herein are methods for treating and/or preventing a cancer in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having cancer characterized by particular gene mutation(s) or variant(s) relative to the genes of a biological wild-type sample. | 2015-04-09 |
| 20150099755 | NOVEL FLUOROERGOLINE ANALOGS - Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT | 2015-04-09 |
| 20150099756 | PYRIMIDINONE COMPOUNDS FOR USE IN THE TREATMENT OF DISEASES OR CONDITIONS MEDIATED BY LP-PLA2 - The present invention relates to novel compounds that inhibit Lp-PLA | 2015-04-09 |
| 20150099757 | PYRIDAZINONE COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS AND METHODS OF TREATING DISORDERS - The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. | 2015-04-09 |
| 20150099758 | Alpha 7 Nicotinic Acetylcholine Receptor Allosteric Modulators, Their Derivatives and Uses Thereof - The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I. | 2015-04-09 |
| 20150099759 | POTENT ANTICANCER ACTIVITY VIA DUAL COMPOUND ACTIVATION - The invention provides compositions and methods for the induction of cell death, for example, cancer cell death. Combinations of compounds and related methods the use are disclosed, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells. The disclosed drug combinations can have lower neurotoxicity effects than other compounds and combinations of compounds. | 2015-04-09 |
| 20150099760 | SALT(S) OF 7-CYCLOPENTYL-2-(5-PIPERAZIN-1-YL-PYRIDIN-2-YLAMINO)-7H-PYRROLO- [2,3-D]PYRIMIDINE-6-CARBOXYLIC ACID DIMETHYLAMIDE AND PROCESSES OF MAKING THEREOF - This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salts thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same. | 2015-04-09 |
| 20150099761 | MODULATORS OF FATTY ACID AMIDE HYDROLASE - 4-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1-carboxylic acid (4-chloro-pyridin-3-yl)-amide is described, which is useful as a FAAH modulator. 4-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1-carboxylic acid (4-chloro-pyridin-3-yl)-amide may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). A method of synthesizing 4-(2,2-difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1-carboxylic acid (4-chloro-pyridin-3-yl)-amide is also disclosed. | 2015-04-09 |
| 20150099762 | COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS - This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity. | 2015-04-09 |
| 20150099763 | ITRACONAZOLE COMPOSITIONS AND DOSAGE FORMS, AND METHODS OF USING THE SAME - The disclosure relates to, among other things, pharmaceutical compositions, such as solid oral dosage forms, comprising itraconazole, methods of making the compositions, and methods of using the same for treating disorders including, but not limited to, fungal infections. | 2015-04-09 |
| 20150099764 | DENDRIMER LIKE AMINO AMIDES POSSESSING SODIUM CHANNEL BLOCKER ACTIVITY FOR THE TREATMENT OF DRY EYE AND OTHER MUCOSAL DISEASES - Sodium channel blockers represented by the formula: | 2015-04-09 |
| 20150099765 | Compounds and Compositions for Cognition-Enhancement, Methods of Making, and Methods of Treating - Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function. | 2015-04-09 |
| 20150099766 | Novel halogen-substituted compounds - The invention relates to compounds of the general formula (I), | 2015-04-09 |
| 20150099767 | SUSTAINED DELIVERY FORMULATIONS OF RISPERIDONE COMPOUNDS - The present invention relates to a risperidone sustained release delivery system for treatment of medical conditions relating delusional psychosis, schizophrenia, bipolar disorder, psychotic depression, obsessive-compulsion disorder, Tourette syndrome, and autistic spectrum disorders. The sustained release delivery system includes a flowable composition containing risperidone, a metabolite, or a prodrug thereof and an implant containing risperidone, a metabolite, or a prodrug thereof. The flowable composition may be injected into tissue whereupon it coagulates to become the solid or gel, monolithic implant. The flowable composition includes a biodegradable, thermoplastic polymer, an organic liquid, and risperidone, a metabolite, or a prodrug thereof. | 2015-04-09 |
| 20150099768 | NOVEL PHARMACEUTICAL FORMULATIONS - There is provided inter alia a dry powder pharmaceutical formulation for inhalation comprising: (i) 6-(2-((4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl) methyl)-3-(2-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-5-yl)-N,N-bis(2-methoxyethyl)hex-5-ynamide or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof and solvates thereof in particulate form as active ingredient; (ii) particulate lactose as carrier; and (iii) a particulate stabilizing agent selected from metal salts of stearic acid such as magnesium stearate and metal salts of stearyl fumarate. | 2015-04-09 |
| 20150099769 | PYRROLO[3,2-D]PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE IN THERAPY - There are disclosed novel compounds of formula (I) | 2015-04-09 |
| 20150099770 | CARBOXYLIC ACID COMPOUNDS - The present disclosure concerns at least one entity chosen from compounds of Formula (I) and pharmaceutically acceptable salts thereof: (I) wherein the variable groups X, R1, R2, R3 m, n and p are as defined herein. The present disclosure also relates to methods for the preparation of at least one such entity, and intermediates useful in the preparation thereof, to pharmaceutical compositions containing at least one such entity, to the use of at least one such entity in the preparation of medicaments, and to the use of at least one such entity in the treatment of conditions such as, for example, allergic diseases, autoimmune diseases, viral diseases, and cancer. | 2015-04-09 |
| 20150099771 | PYRIDINE CGRP RECEPTOR ANTAGONISTS - The present invention is directed to pyridine derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved. | 2015-04-09 |
| 20150099772 | SUBSTITUTED BERBINES AND THEIR SYNTHESIS - The present invention provides substituted berbines, processes for the synthesis of substituted berbine compounds, as well as intermediates used in the synthesis of substituted berbine compounds. Also provided are methods for using the substituted berbines to inhibit cancer cell growth. | 2015-04-09 |
| 20150099773 | PROCESS FOR THE PREPARATION OF QUATERNARY N-ALKYL MORPHINAN ALKALOID SALTS - An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives. | 2015-04-09 |
| 20150099774 | Pyrido [3,4-C] [1,9] phenanthroline and 11, 12 dihydropyrido [3,4-C] [1,9] phenanthroline derivatives and the use thereof, particularly for treating cancer - New phenanthroline derivatives as drug as well as methods for producing said compounds are provided. | 2015-04-09 |
| 20150099775 | COMPOSITIONS AND METHODS FOR TREATING CANCERS - The present invention relates to compositions and methods for treating of cancer. In some embodiments, the invention relates to the use of agents that can modulate a component in the CDX2-KLF4 signaling pathway to treat myelodysplastic syndromes (MDS), acute myelogenous leukemia (AML), acute lymphocytic leukemia (ALL), adult T-cell leukaemia (ATLL), lymphoma, gastric cancer, multiple myeloma, or combinations thereof, or a condition associated with abnormal activity of the CDX2-KLF4 signaling pathway. | 2015-04-09 |
| 20150099776 | Beta-Amyloid-Directed Multitarget Compounds For The Treatment Of Alzheimer's Disease - The compounds of formula (I), or its pharmaceutically acceptable salts, or any stereoisomer or mixture thereof, wherein: R | 2015-04-09 |
| 20150099777 | HETEROCYCLIC COMPOUND - A compound having an SSTR5 antagonist action and use of the compound as a medicament are provided. Specifically, a compound represented by the following formula: | 2015-04-09 |
| 20150099779 | ROR MODULATORS AND THEIR USES - The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR. | 2015-04-09 |
| 20150099780 | DEUTERATED CFTR POTENTIATORS - This invention relates to compounds of Formula I: | 2015-04-09 |
| 20150099781 | Compounds and Methods for Treating Mammalian Gastrointestinal Microbial Infections - Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants. | 2015-04-09 |
| 20150099782 | ANTAGONISTS OF PROSTAGLANDIN EP3 RECEPTOR - Provided herein are antagonists of prostaglandin EP3 receptor, processes to make said antagonists, and methods comprising administering said antagonists to a mammal in need thereof. | 2015-04-09 |
| 20150099783 | USE OF CCR3-INHIBITORS - The present invention relates to CCR3 inhibitors of formula 1, | 2015-04-09 |
| 20150099784 | PIPERAZINE, PIPERIDINE AND TETRAHYDROPYRIDINE DERIVATIVES AND THEIR PHARMACEUTICAL USE - Novel piperazine, piperidine and tetrahydropyridine derivatives comprising a dibenzofurane moiety are provided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof. | 2015-04-09 |
| 20150099785 | STABILIZED EFINACONAZOLE COMPOSITIONS - The present invention provides compositions containing efinaconazole, butylated hydroxytoluene, a salt of ethylenediaminetetraacetic acid, and optional citric acid. The compositions exhibit stable color profiles and are useful in the treatment of fungal infections. | 2015-04-09 |
| 20150099786 | CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS - The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. | 2015-04-09 |
| 20150099787 | Non-Flushing Niacin Analogues, and Methods of Use Thereof - One aspect of the present invention relates to substituted pyridines and pharmaceutially acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels. | 2015-04-09 |
| 20150099788 | CONTROLLED RELEASE ORAL FORMULATIONS OF ION CHANNEL MODULATING COMPOUNDS AND RELATED METHODS FOR PREVENTING ARRHYTHMIA - The present invention provides methods of treating and preventing arrhythmia and other diseases or disorders, using ion channel modulating compounds, including vernakalant hydrochloride. The present invention further provides controlled release oral formulations and dosages of vernakalant hydrochloride, which are effective in preventing arrhythmia. Certain methods and formulations of the present invention are adapted for the treatment and prevention of arrhythmia and other disease or disorders in subjects identified as having altered drug metabolism due to polymorphism of the gene encoding cytochrome P450 2D6. | 2015-04-09 |
| 20150099789 | Use of Odiparcil in the Treatment of a Mucopolysaccharidosis - The present invention relates to a method of treatment of a mucopolysaccharidosis with 4-methyl-2-oxo-2H-1-benzopyran-7-yl-5-thio-β-D-xylopyranoside. | 2015-04-09 |
| 20150099790 | COMPOSITIONS AND METHODS FOR MODULATING MITOCHONDRIAL PYRUVATE CARRIER ACTIVITY - Disclosed herein are methods and compositions for the diagnosis and treatment of conditions associated with aberrant pyruvate metabolism, and symptoms thereof, in a subject. Disclosed herein are methods of detecting an aberrant pyruvate metabolism-associated condition, and symptoms thereof, in a subject, by the expression level of MPC1 or MPC2. Disclosed herein are methods of detecting an aberrant pyruvate metabolism-associated condition, and symptoms thereof, in a subject, by the activity level of MPC1 or MPC2. Disclosed herein are methods of determining responsiveness to a treatment for an aberrant pyruvate metabolism associated condition, and symptoms thereof, in a subject. | 2015-04-09 |
| 20150099791 | COMPOSITIONS AND METHODS FOR MODULATING UTRN EXPRESSION - Aspects of the invention provide single stranded oligonucleotides for activating or enhancing expression of UTRN. Further aspects provide compositions and kits comprising single stranded oligonucleotides for activating or enhancing expression of UTRN. Methods for modulating expression of UTRN using the single stranded oligonucleotides are also provided. Further aspects of the invention provide methods for selecting a candidate oligonucleotide for activating or enhancing expression of UTRN. | 2015-04-09 |
| 20150099792 | ANTISENSE MODULATION OF GCGR EXPRESSION - Provided herein are methods, compounds, and compositions for reducing expression of GCGR mRNA and protein in an animal. Such methods, compounds, and compositions are useful to treat, prevent, delay, or ameliorate metabolic disease, for example, diabetes, or a symptom thereof. | 2015-04-09 |
| 20150099793 | RATIONAL DESIGN OF microRNA-siRNA CHIMERAS FOR MULTI-FUNCTIONAL TARGET SUPPRESSION - The present disclosure encompasses methods for rational design of microRNA and small interfering RNA chimeras and compositions and methods of use thereof. | 2015-04-09 |
| 20150099794 | GNAQ TARGETED dsRNA COMPOSITIONS AND METHODS FOR INHIBITING EXPRESSION - The invention relates to a double-stranded ribonucleic acid (dsRNA) targeting a G-alpha q subunit (GNAQ) of a heterotrimeric G gene, and methods of using the dsRNA to inhibit expression of GNAQ. | 2015-04-09 |
| 20150099795 | THERAPEUTIC AGENT FOR TREATING TRYPANOSOMA-ASSOCIATED DISEASE, METHOD FOR KILLING TRYPANOSOMA PARASITES, AND USE THEREOF - A therapeutic agent for treating a | 2015-04-09 |
| 20150099796 | Compositions and Methods for Gene Silencing - Compositions and methods for modulating the expression of a protein of interest are provided. | 2015-04-09 |
| 20150099797 | OLIGONUCLEOTIDE COMPOSITIONS WITH ENHANCED EFFICIENCY - The oligonucleotide compositions of the present invention make use of combinations of oligonucleotides. In one aspect, the invention features an oligonucleotide composition including at least 2 different oligonucleotides targeted to a target gene. This invention also provides methods of inhibiting protein synthesis in a cell and methods of identifying oligonucleotide compositions that inhibit synthesis of a protein in a cell. | 2015-04-09 |
| 20150099798 | VARIANTS OF YEAST NDI1 GENE, AND USES THEREOF IN THE TREATMENT OF DISEASE ASSOCIATED WITH MITOCHONDRIAL DYSFUNCTION - An isolated nucleic acid sequence encoding the yeast NDI1 protein of SEQ ID NO: 542 or a functional variant thereof is described. The nucleic acid sequence comprises at least 50 codons which are codon optimised compared with the sequence of yeast NDI1 gene of SEQ ID NO: 1. | 2015-04-09 |
